There is a need to explain that generic versions of a drug may not be manufactured by the same process as brand-name drugs and that the different processes may have dramatically different environmental impacts. Two global forces are at odds today—the push for "greener" processes and the push for lower drug prices. This book brings this conflict into sharp focus by discussing in detail the published process chemistry for top-selling small molecule drugs. Providing insights about process route selection, choice of reagents, and reaction conditions, Pharmaceutical Process Chemistry for Synthesis guides process chemists in identifying best processes for manufacturing these blockbuster drugs as they lose patent protection. Further, it highlights the strategies and methodology that might be useful for expediting the process research and development of the blockbusters of the future. Written from a refreshingly objective perspective, this book is essential for process chemists who need to devise practical syntheses for increasingly complex drugs in a constantly decreasing time frame.

Covering the whole area of process chemistry in the pharmaceutical industry, this monograph provides the essential knowledge on the basic chemistry needed for future development and key industrial techniques, as well as morphology, engineering and regulatory compliances. Application-oriented and well structured, the authors include recent examples of excellent industrial production of active pharmaceutical ingredients.

Providing guidance for chemists and other scientists entering pharmaceutical discovery and development, this up-to-the-minute reference presents contributions from an international group of nearly 50 renowned researchers—offering a solid grounding in synthetic and physical organic chemistry, and clarifying the roles of various specialties in the development of new drugs. Featuring over 1000 references, tables, and illustrations, Process Chemistry in the Pharmaceutical Industry is sure to find its way to the bookshelves of organic, physical, analytical, process, and medicinal chemists and biochemists; pharmacists; and upper-level undergraduate and graduate students in these disciplines.

As pharmaceutical companies strive to develop safer medicines at a lower cost, they must keep pace with the rapid growth of technology and research methodologies. Defying the misconception of process chemistry as mere scale-up work, Process Chemistry in the Pharmaceutical Industry, Vol. 2: Challenges in an Ever Changing Climate explor

Introduction to Drug Synthesis explores the central role played by organic synthesis in the process of drug design and development - from the generation of novel drug structures to the improved efficiency of large scale synthesis.

Pharmaceutical process research and development is an exacting, multidisciplinary effort but a somewhat neglected discipline in the chemical curriculum. This book presents an overview of the many facets of process development and how recent advances in synthetic organic chemistry, process technology and chemical engineering have impacted on the manufacture of pharmaceuticals. In 15 concise chapters the book covers such diverse subjects as route selection and economics, the interface with medicinal chemistry, the impact of green chemistry, safety, the crucial role of physical organic measurements in gaining a deeper understanding of chemical behaviour, the role of the analyst, new tools and innovations in reactor design, purification and separation, solid state chemistry and its role in formulation. The book ends with an assessment of future trends and challenges. The book provides a valuable overview of: both early and late stage chemical development, how safe and scaleable synthetic routes are designed, selected and developed, the importance of the chemical engineering, analytical and manufacturing interfaces, the key enabling technologies, including catalysis and biocatalysis, the importance of the green chemical perspective and solid form issues. The book, written and edited by experts in the field, is a contemporary, holistic treatise, with a logical sequence for process development and mini-case histories within the chapters to bring alive different aspects of the process. It is completely pharmaceutical themed, encompassing all essential aspects, from route and reagent selection to manufacture of the active compound. The book is aimed at both graduates and postgraduates interested in a career in the pharmaceutical industry. It informs them about the breadth of the work carried out in chemical research and development departments, and gives them a feel for the challenges involved in the job. The book is also of value to academics who often understand the drug discovery arena, but have far less appreciation of the drug development area, and are thus unable to advise their students about the relative merits of careers in chemical development versus discovery.

Dr. Oljan Repic clearly explains the goals and basic principles of chemical development. He explores the crucial aspects of a new process that must be considered when scaling up a research synthesis to industrial levels. And, with the help of many case studies and vignettes, he delineates each phase of the development process. Key topics include qualities of an ideal process, techniques for minimizing impurities, criteria for cost-effective synthesis of enantiopure compounds by resolutions, asymmetric synthesis and the "chiral pool" strategy, synthesis for labeling substances with hydrogen or carbon isotopes, and new drug registration requirements. This book is an invaluable reference for professionals as well as an important source of guidance and inspiration for young chemists considering entering the field.

Presents the most effective catalytic reactions in use today, with a special focus on process intensification, sustainability, waste reduction, and innovative methods This book demonstrates the importance of efficient catalytic transformations for producing pharmaceutically active molecules. It presents the key catalytic reactions and the most efficient catalytic processes, including their significant advantages over compared previous methods. It also places a strong emphasis on asymmetric catalytic reactions, process intensification (PI), sustainability and waste mitigation, continuous manufacturing processes as enshrined by continuous flow catalysis, and supported catalysis. Active Pharmaceutical Ingredients in Synthesis: Catalytic Processes in Research and Development offers chapters covering: Catalysis and Prerequisites for the Modern Pharmaceutial Industry Landscape; Catalytic Process Design - The Industrial Perspective; Hydrogenation, Hydroformylation and Other Reductions; Oxidation; ; Catalytic Addition Reactions; Catalytic Cross-Coupling Reactions; Catalytic Metathesis Reactions; Catalytic Cycloaddition Reactions: Coming Full-Circle; Catalytic Cyclopropanation Reactions; Catalytic C-H insertion Reactions; Phase Transfer Catalysis; and Biocatalysis. -Provides the reader with an updated clear view of the current state of the challenging field of catalysis for API production -Focuses on the application of catalytic methods for the synthesis of known APIs -Presents every key reaction, including Diels-Alder, CH Insertions, Metal-catalytic coupling-reactions, and many more -Includes recent patent literature for completeness Covering a topic of great interest for synthetic chemists and R&D researchers in the pharmaceutical industry, Active Pharmaceutical Ingredients in Synthesis: Catalytic Processes in Research and Development is a must-read for every synthetic chemist working with APIs.

Designed to provide a comprehensive, step-by-step approach to organic process research and development in the pharmaceutical, fine chemical, and agricultural chemical industries, this book describes the steps taken, following synthesis and evaluation, to bring key compounds to market in a cost-effective manner. It describes hands-on, step-by-step, approaches to solving process development problems, including route, reagent, and solvent selection; optimising catalytic reactions; chiral syntheses; and "green chemistry." Second Edition highlights:• Reflects the current thinking in chemical process R&D for small molecules• Retains similar structure and orientation to the first edition. • Contains approx. 85% new material• Primarily new examples (work-up and prospective considerations for pilot plant and manufacturing scale-up)• Some new/expanded topics (e.g. green chemistry, genotoxins, enzymatic processes)• Replaces the first edition, although the first edition contains useful older examples that readers may refer to - Provides insights into generating rugged, practical, cost-effective processes for the chemical preparation of "small molecules" - Breaks down process optimization into route, reagent and solvent selection, development of reaction conditions, workup, crystallizations and more - Presents guidelines for implementing and troubleshooting processes

Chemistry and chemical engineering have changed significantly in the last decade. They have broadened their scopeâ€"into biology, nanotechnology, materials science, computation, and advanced methods of process systems engineering and controlâ€"so much that the programs in most chemistry and chemical engineering departments now barely resemble the classical notion of chemistry. Beyond the Molecular Frontier brings together research, discovery, and invention across the entire spectrum of the chemical sciencesâ€"from fundamental, molecular-level chemistry to large-scale chemical processing technology. This reflects the way the field has evolved, the synergy at universities between research and education in chemistry and chemical engineering, and the way chemists and chemical engineers work together in industry. The astonishing developments in science and engineering during the 20th century have made it possible to dream of new goals that might previously have been considered unthinkable. This book identifies the key opportunities and challenges for the chemical sciences, from basic research to societal needs and from terrorism defense to environmental protection, and it looks at the ways in which chemists and chemical engineers can work together to contribute to an improved future.